EGFR Inhibitor

EGFR-IN-12 (Standard) is the analytical standard of EGFR-IN-12. This product is intended for research and analytical applications. EGFR-IN-12 is a 4,6-disubstituted pyrimidine and is a potent, ATP-competitive, irreversible and highly selective EGFR inhibitor with an IC50of 21 nM. EGFR-IN-12 also inhibits mutant EGFRL858R and EGFRL861Q with IC50s of 63 nM and 4 nM, respectively. EGFR-IN-12 displays strong selectivity for EGFR over HER4 (IC50 = 7640 nM) and a panel of 55 other kinases. EGFR-IN-12 induces cells apoptosis and has antitumor activity.

Falnidamol (Standard) is the analytical standard of Falnidamol. This product is intended for research and analytical applications. Falnidamol (BIBX 1382) is an orally active, selective EGFR tyrosine kinase inhibitor with an IC50 of 3 nM. Falnidamol displays > 1000-fold lower potency against ErbB2 (IC50=3.4 μM) and a range of other related tyrosine kinases (IC50>10 μM). Falnidamol is a pyrimido-pyrimidine compound and has anti-cancer activity.

Simotinib (Standard) is the analytical standard of Simotinib. This product is intended for research and analytical applications. Simotinib is a selective, specific, and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 19.9 nM. Antineoplastic activities.

Lavendustin C6 is a specific inhibitor of tyrosine kinase. Lavendustin C6 inhibits epidermal growth factor (EGF) receptor tyrosine kinase with an EC₅₀ value of 0.05 μg/mL. Lavendustin C6 inhibits platelet-derived growth factor (PDGF)-induced inositol phosphate formation.

ALK-IN-1 (Standard) is the analytical standard of ALK-IN-1 (Brigatinib analog) (HY-13464). This product is intended for research and analytical applications. ALK-IN-1 is an ALK and EGFR inhibitor. ALK-IN-1 binds to and inhibits ALK kinase, ALK fusion proteins, and wild-type and mutant EGFR variants, thereby disrupting their corresponding signaling pathways. ALK-IN-1 can suppress the growth and proliferation of tumor cells and exhibits potential inhibitory activity against mutant EGFR. ALK-IN-1 can be used in the research of non-small-cell lung cancer.

EAI045 (Standard) is the analytical standard of EAI045 (HY-100213). This product is intended for research and analytical applications. EAI045 is an allosteric and the fourth-generation inhibitor of mutant EGFR with IC50s of 1.9, 0.019, 0.19 and 0.002 μM for EGFR, EGFRL858R, EGFRT790M and EGFRL858R/T790M at 10 μM ATP, respectively.

D-69491 hydrochloride is a HER-2 tyrosine kinase inhibitor that reduces HER-2 phosphorylation, inhibits the proliferation of SKOV-3 cells, and has anticancer activity.

Gefitinib (hydrochloride) (Standard) is the analytical standard of Gefitinib (hydrochloride). This product is intended for research and analytical applications. Gefitinib hydrochloride (ZD1839 hydrochloride) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib hydrochloride selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib hydrochloride also induces autophagy. Gefitinib hydrochloride has antitumour activity.

CDKi free base is a CDK inhibitor. CDKi free base induces morphological changes, DNA fragmentation, and cell death in vestibular schwannoma cells. CDKi free base downregulates pRb, EGF-R, PI3K, NF-κB, and Shh levels, while upregulating JNK, ASK1, Caspase 3, and p21, and induces PARP-1 cleavage. CDKi free base can be used in research related to vestibular schwannoma.

DMBT is an orally effective anti-tumor metastasis and anti-angiogenesis agent. DMBT downregulates key molecules such as EGFR/p-Akt/HIF-1α/VEGF/MMP-9, inhibits the HIF-1α/VE-cadherin (cadherin)/MMPs and Nrf2/HO-1 signaling pathways, and reduces hypoxia-induced ROS levels as well as the secretion and activity of MMP-9. DMBT inhibits hypoxia-induced vasculogenic mimicry, cancer cell migration, invasion and metastasis, and exhibits no obvious cytotoxicity to normal cells. DMBT reduces the area of laser-induced choroidal neovascularization lesions. DMBT can be used in studies related to breast cancer, melanoma and macular degeneration.

Paeciloquinone A can inhibit EGFR protein tyrosine kinase. Paeciloquinone A inhibits the V-abl protein tyrosine kinase with an IC₅₀ of 0.59 μM.

CL-387785 (EKI-785; WAY-EKI 785) (Standard) is the analytical standard of CL-387785 (HY-10325). This product is intended for research and analytical applications. CL-387785 is an orally active EGFR inhibitor with an IC₅₀ of 370 pM. CL-387785 inhibits EGF-stimulated EGFR autophosphorylation with an IC₅₀ of approximately 5 nM. CL-387,785 exerts selective inhibition on cell lines overexpressing EGFR or c-erbB-2, whereas it shows weak inhibitory effects on cell lines with low expression of these two receptors. CL-387785 effectively induces cell cycle arrest and apoptosis. CL-387785 can be used for the research of non-small cell lung cancer and autosomal recessive polycystic kidney disease.

Paeciloquinone B can inhibit the EGFR protein tyrosine kinase.

LDC0496 is a potent and selective EGFR inhibitor. LDC0496 possesses intense inhibitory potency toward EGFR and Her2 exon20 insertion mutations, as well as selectivity over wild type EGFR and within the kinome.